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BIO-acetoxime

Catalog No. T6787 CAS 667463-85-6

Synonyms: BIA, GSK-3 Inhibitor X

BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, <240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.

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BIO-acetoxime, CAS 667463-85-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 115.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 396.00
100 mg	In stock	$ 589.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 97.28%

Biological Description

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Description	BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.
Targets&IC50	GSK-3α:10 nM, GSK-3β:10 nM
In vitro	In human oral epithelial cells, BIO-acetoxime suppresses viral gene expression and protects oral epithelial cells from HSV-1 infection. [2] In SY5Y-MYCN cells, BIO-acetoxime strongly reduces c-MYC expression and p-SMAD3 levels. BIO-acetoxime also decreases cell viability of KCN, KCNR, SY5Y, Kelly, and IMR32 cells by mediating apoptosis. [3] In HEK 293T cells, BIO-acetoxime is also found to reduce antiviral innate immunity downstream of IRF3 activation by inhibition of GSK3α/β activities. [4]
Kinase Assay	Kinase Assays: Kinases activities are assayed in Buffer A or C, at 30 °C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated for a 10 min incubation. The activities are expressed in % of the maximal activity, i.e., in the absence of inhibitors. Controls are performed with appropriate dilutions of DMSO. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/mL 10 mM DTT, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-33P] ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 30 min incubation at 30 °C, 25 μL aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and, 20 s later, the filters are washed five times (for at least 5 min each time) in a solution of 10 mL phosphoric acid/liter of water. The wet filters are counted in the presence of 1 mL of ACS scintillation fluid. CDK1/cyclin B is extracted in homogenization buffer from M phase starfish (Marthasterias glacialis) oocytes and purified by affinity chromatography on p9CKShs1-sepharose beads, from which it is eluted by free p9CKShs1. The kinase activity is assayed in buffer C, with 1 mg histone H1 /mL, in the presence of 15 μM [γ-32P] ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 10 min incubation at 30 °C, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. CDK5/p25 is reconstituted by mixing equal amounts of recombinant mammalian CDK5 and p25 expressed in E. coli as GST (Glutathione-S-transferase) fusion proteins and purified by affinity chromatography on glutathione-agarose (p25 is a truncated version of p35, the 35 kDa CDK5 activator). Its activity is assayed in buffer C as described for CDK1/cyclin B.0
Cell Research	Cell viability is analyzed by CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer's instructions, approximately 5,000 cells are plated per well of 96-well tissue culture plates with 100 μL of medium. To assess cell viability, rather than proliferation rate, inhibitor- and control-treated cells are assayed after the same growth time had elapsed. The results represent the mean ± SD of triplicate samples, expressed as a percentage of control.(Only for Reference)

Synonyms	BIA, GSK-3 Inhibitor X
Molecular Weight	398.21
Formula	C18H12BrN3O3
CAS No.	667463-85-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 8 mg/mL (20 mM)

References and Literature

1. Polychronopoulos P, et al. J Med Chem. 2004, 47(4), 935-946. 2. Hsu MJ, et al. Arch Virol. 2013, 158(6), 1287-1296. 3. Duffy DJ, et al. Mol Cancer Ther. 2014, 13(2), 454-467. 4. Khan KA, et al. Mol Cell Biol. 2015, 35(17), 3029-3043.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library NO PAINS Compound Library PI3K-AKT-mTOR Compound Library Anti-Diabetic Compound Library Reprogramming Compound Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BIO-acetoxime 667463-85-6 Apoptosis Microbiology/Virology PI3K/Akt/mTOR signaling Stem Cells GSK-3 HSV BIO acetoxime Glycogen synthase kinase 3 BIA inhibit Herpes simplex virus Glycogen synthase kinase-3 GSK-3 Inhibitor X Inhibitor BIOacetoxime inhibitor

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